Citation: Liu Jun, Hou Jinsong, Meng Ying, Miao Zhiying, Lin Jing, Chen Weimin. Research Progress of Antibiotics Conjugated with Siderophores[J]. Chinese Journal of Organic Chemistry, ;2020, 40(10): 3026-3043. doi: 10.6023/cjoc202006042 shu

Research Progress of Antibiotics Conjugated with Siderophores

College of Pharmacy, Jinan University, Guangzhou 510632

Corresponding author: Chen Weimin, twmchen@jnu.edu.cn
Received Date: 21 June 2020
Revised Date: 20 August 2020
Available Online: 26 August 2020
Fund Project: the National Natural Science Foundation of China 81872776Project supported by the National Natural Science Foundation of China (No. 81872776)

Figures(19)

The natural siderophore is a class of small-molecule iron ion chelating agents secreted by bacteria, which can be recognized by specific outer membrane receptors and transported into cytoplasm to provide iron for bacteria. Using this characteristic of siderophore, antibiotics can be coupled with them and enter into bacteria through the bacterial iron uptake system. This strategy is called "Trojan horse" strategy. Recently, cefiderocol, the first siderophore-antibiotic conjugate, was approved for marketing, which has aroused accumulated interest of scientists and pharmaceutical companies in this field. This paper provides a comprehensive review of the progress in antibiotics conjugated with siderophores from three aspects:the types of siderophore molecules, antibiotics with different action mechanisms, and the role of linkers. The basic relationship between anti-bacterial activity and three moieties of this novel type of anti-bacterial agents has been revealed. This review will provide a reference for the development of new antibiotics conjugated with siderophores.
- antibiotic,
- siderophore,
- conjugate,
- "Trojan horse" strategy
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沈阳化工大学材料科学与工程学院沈阳 110142